714971-09-2 Usage
Description
AC480 (BMS-599626) is a highly selective pan-HER kinase inhibitor with IC50 values of 20 and 30 nM for the inhibition of HER1 and HER2, respectively. It is a potent inhibitor of HER1 and HER2 kinases and modulates receptor signaling to inhibit tumor cell proliferation.
Used in Pharmaceutical Industry:
AC480 (BMS-599626) is used as an anticancer agent for inhibiting the proliferation of tumor cells by modulating HER1 and HER2 receptor signaling. It inhibits HER1/HER2 receptor heterodimerization, providing an additional mechanism of inhibiting tumors in which receptor coexpression and heterodimerization play a major role in driving tumor growth.
Biological Activity
ac480 (bms-599626) is a potent, selective inhibitor of human epidermal growth factor receptor (her) that inhibits her1 and her2 with ic values of 20 nm and 30 nm, respectively. ac480 has been proved to inhibit her1 in an atp-competitive manner. on the contrary, ac480 has shown to be an atp noncompetitive inhibitor of her2 [1]ac480 inhibited the proliferation of sal2 cells derived from a transgenic mouse tumor, breast tumor and gastric carcinoma cell lines, geo colon tumor cells, non–small-cell lung tumor cells line via her1 and/or her2 signalings [1].ac480 by oral administration has been demonstrated to suppress the growth of sal2 tumor, geo xenograft tumor, kpl-4 and bt474 breast tumors, n87 gastric tumor, a549 and l2987 non–small-cell lung tumors in nude mice [1].
references
[1] wong tw1, lee fy, yu c, luo fr, oppenheimer s, zhang h, smykla ra, mastalerz h, fink be, hunt jt,gavai av, vite gd. preclinical antitumor activity of bms-599626, a pan-her kinase inhibitor that inhibits her1/her2 homodimer and heterodimer signaling. clin cancer res. 2006 oct 15;12(20 pt 1):6186-93.
Check Digit Verification of cas no
The CAS Registry Mumber 714971-09-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,1,4,9,7 and 1 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 714971-09:
(8*7)+(7*1)+(6*4)+(5*9)+(4*7)+(3*1)+(2*0)+(1*9)=172
172 % 10 = 2
So 714971-09-2 is a valid CAS Registry Number.
714971-09-2Relevant articles and documents
SYNTHETIC PROCESS
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, (2008/06/13)
The present invention provides a process for preparing compounds of formula (I) ["insert chemical structure here"](I)or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.